Patents by Inventor Matthew Allen Zajac
Matthew Allen Zajac has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20160168168Abstract: The present invention is a process comprising contacting a compound of formula 6: or a pharmaceutically acceptable salt thereof; with a deprotecting reagent to form a compound of formula A: or a pharmaceutically acceptable salt thereof; where R is H or OR1; R1 and each R1? are protecting groups; R1? is H or OH, and n is 0, 1, 2, 3, 4, or 5.Type: ApplicationFiled: December 15, 2015Publication date: June 16, 2016Inventors: Jose J. CONDE, John Anthony KOWALSKI, Matthew Allen ZAJAC
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Patent number: 9243003Abstract: The present invention is a process comprising contacting a compound of formula 6: or a pharmaceutically acceptable salt thereof; with a deprotecting reagent to form a compound of formula A: or a pharmaceutically acceptable salt thereof; where R is H or OR1; R1 and each R1? are protecting groups; R1? is H or OH, and n is 0, 1, 2, 3, 4 , or 5.Type: GrantFiled: April 6, 2011Date of Patent: January 26, 2016Assignee: GlaxoSmithKline LLCInventors: Jose J. Conde, John Anthony Kowalski, Matthew Allen Zajac
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Patent number: 8759542Abstract: The present application provides a process for the preparation of ?-carboxamide pyrrolidine derivatives of formula (I), wherein R1 and R2 are independently hydrogen, C1-6alkyl or C3-6cycloalkylC1-6alkyl; or such R1 and R2, together with the nitrogen to which they are attached, may form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R5 is independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; either R6 or R7 is —O—R8, —OCHR9R8, —NCH2R8 or —(CH2)2R8 wherein the other R6 or R7 is hydrogen or R5; and wherein R8 is a phenyl ring or wherein the phenyl ring is optionally substituted by one or more groups independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; and R9 is hydrogen or C1-3alkyl.Type: GrantFiled: September 1, 2010Date of Patent: June 24, 2014Assignee: Convergence Pharmaceuticals LimitedInventor: Matthew Allen Zajac
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Publication number: 20130035501Abstract: The present invention is a process comprising contacting a compound of formula 6: or a pharmaceutically acceptable salt thereof; with a deprotecting reagent to form a compound of formula A: or a pharmaceutically acceptable salt thereof; where R is H or OR1; R1 and each R1? are protecting groups; R1? is H or OH, and n is 0, 1, 2, 3, 4, or 5.Type: ApplicationFiled: April 6, 2011Publication date: February 7, 2013Applicant: GLAXOSMITHKLINE LLCInventors: Jose J. Conde, John Anthony Kowalski, Matthew Allen Zajac
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Publication number: 20120226053Abstract: The present application provides a process for the preparation of ?-carboxamide pyrrolidine derivatives of formula (I), wherein R1 and R2 are independently hydrogen, C1-6alkyl or C3-6cycloalkylC1-6alkyl; or such R1 and R2, together with the nitrogen to which they are attached, may form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R5 is independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; either R6 or R7 is —O—R8, —OCHR9R8,—NCH2R8 or —(CH2)2R8 wherein the other R6 or R7 is hydrogen or R5; and wherein R8 is a phenyl ring or wherein the phenyl ring is optionally substituted by one or more groups independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; and R9 is hydrogen or C1-3alkyl.Type: ApplicationFiled: September 1, 2010Publication date: September 6, 2012Inventor: Matthew Allen Zajac
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Patent number: 8076475Abstract: The present invention generally relates to a novel process for preparing vitronectin receptor antagonist compounds having a benzodiazepinyl core structure. This invention relates to the preparation of pharmaceutically active compounds which inhibit the vitronectin receptor and are useful for treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporosis. In particular, the present invention relates to a novel process for preparing (±)-3-oxo-8-{[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid, (R)-3-oxo-8-{[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid and (S)-3-oxo-8-{[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 6, 2009Date of Patent: December 13, 2011Assignee: GlaxoSmithKline LLCInventor: Matthew Allen Zajac
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Publication number: 20110166170Abstract: The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The ?,?-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores.Type: ApplicationFiled: October 27, 2010Publication date: July 7, 2011Applicant: President and Fellows of Harvard CollegeInventors: Andrew G. Myers, Seth B. Herzon, Jeremy Earle Wulff, Romain Siegrist, Jakub Svenda, Matthew Allen Zajac
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Patent number: 7902196Abstract: The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The ?,?-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores.Type: GrantFiled: March 17, 2006Date of Patent: March 8, 2011Assignee: President and Fellows of Harvard CollegeInventors: Andrew G. Myers, Seth B. Herzon, Jeremy Earle Wulff, Romain Siegrist, Jakub Svenda, Matthew Allen Zajac
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Publication number: 20110015390Abstract: The present invention generally relates to a novel process for preparing vitronectin receptor antagonist compounds having a benzodiazepinyl core structure. This invention relates to the preparation of pharmaceutically active compounds which inhibit the vitronectin receptor and are useful for treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporosis. In particular, the present invention relates to a novel process for preparing (±)-3-oxo-8-{[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid, (R)-3-oxo-8-{[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid and (S)-3-oxo-8-{[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 6, 2009Publication date: January 20, 2011Inventor: Matthew Allen Zajac